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    Pyrimidine derivatives
    1.
    发明授权
    Pyrimidine derivatives 失效
    嘧啶衍生物

    公开(公告)号：US4851519A

    公开(公告)日：1989-07-25

    申请号：US080021

    申请日：1987-07-31

    申请人： Robert W. Lambert ,  Joseph A. Martin ,  Gareth J. Thomas

    发明人： Robert W. Lambert ,  Joseph A. Martin ,  Gareth J. Thomas

    IPC分类号： C07D405/04 ,  A61K31/505 ,  A61P31/12 ,  C07D405/14 ,  C07D409/14 ,  C07H19/06

    CPC分类号： C07H19/06

    摘要： Compounds of the formula ##STR1## wherein R.sup.1 is halogen, C.sub.1-4 -alkyl, halo-(C.sub.1-4 -alkyl) or C.sub.2-4 -alkanoyl,R.sup.2 is hydrogen, hydroxy, C.sub.1-4 alkoxy, C.sub.1-4 -alkylthio or phenyl-(C.sub.1-4 -alkoxy) or , when X is O, also acyloxy,R.sup.3 is hydrogen or C.sub.1-4 -alkyl,R.sup.4 is a carbocyclic group or a heterocyclic group,R.sup.5 is hydrogen or fluorine,m stands for zero, 1 or 2,X is O or NH and Y is a direct bond, --CH.dbd.CH--, --C.tbd.C-- or a group of the formula of--(Z).sub.n --A-- (a)in which A is a C.sub.1-8 alkylene group which is optionally substituted by one or two phenyl groups,Z is O, S, SO or SO.sub.2 and n stands for zero or 1, with the proviso that R.sup.1 is different from iodine, when R.sup.2 is hydroxy or benzoyloxy, R.sup.3 is hydrogen,R.sup.4 is unsubstituted phenyl, R.sup.5 is hydrogen, m stands for zero, X is O, and Y is a direct bond, and tautomers thereof, which possess antiviral activity and can therefore be used in the form of medicaments for the control and prevention of viral infections are described. The compounds of formula I can be prepared according to known methods.

    摘要翻译： 式Ⅰ化合物其中R1是卤素，C1-4烷基，卤代（C1-4烷基）或C2-4-烷酰基，R2是氢，羟基，C1-4烷氧基，C1-4烷硫基 或苯基 - （C 1-4 - 烷氧基），或者当X是O时也是酰氧基，R 3是氢或C 1-4 - 烷基，R 4是碳环基或杂环基，R 5是氢或氟，m代表0 ，1或2，X是O或NH，Y是直接键，-CH = CH-，-C 3BOND C-或 - 式（Z）nA（a）的基团，其中A是C1 -8亚烷基，其任选被一个或两个苯基取代，Z是O，S，SO或SO 2，n代表0或1，条件是R1不同于碘，当R2是羟基或苯甲酰氧基时，R3是 氢，R4是未取代的苯基，R5是氢，m代表0，X是O，Y是直接键，其互变异构体具有抗病毒活性，因此可以以用于控制和预防的药物的形式使用 描述了病毒感染。 式I化合物可以根据已知方法制备。

    Method of treating herpes simplex viral infection employing pyrimidine derivatives
    2.
    发明授权
    Method of treating herpes simplex viral infection employing pyrimidine derivatives 失效
    使用嘧啶衍生物治疗单纯疱疹病毒感染的方法

    公开(公告)号：US5010060A

    公开(公告)日：1991-04-23

    申请号：US342277

    申请日：1989-04-24

    申请人： Robert W. Lambert ,  Joseph A. Martin ,  Gareth J. Thomas

    发明人： Robert W. Lambert ,  Joseph A. Martin ,  Gareth J. Thomas

    IPC分类号： C07D405/04 ,  A61K31/505 ,  A61P31/12 ,  C07D405/14 ,  C07D409/14 ,  C07H19/06

    CPC分类号： C07H19/06

    摘要： Compounds of the formula ##STR1## wherein R.sup.1 is halogen, C.sub.1-4 -alkyl, halo-(C.sub.1-4 -alkyl) or C.sub.2-4 -alkanoyl,R.sup.2 is hydrogen, hydroxy, C.sub.1-4 -alkoxy, C.sub.1-4 -alkylthio or phenyl-(C.sub.1-4 -alkoxy) or, when X is O, also acyloxy,R.sup.3 is hydrogen or C.sub.1-4 -alkyl,R.sup.4 is a carbocyclic group or a heterocyclic group,R.sup.5 is hydrogen or fluorine,m stands for zero, 1 or 2,X is O or NH and Y is a direct bond, --CH.dbd.CH--, --C.tbd.C-- or a group of the formula of--(Z).sub.n --A-- (a) in which A is a C.sub.1-8 -alkylene group which is optionally substituted by one or two phenyl groups, is O, S, SO or SO.sub.2 and n stands for zero or 1, with the proviso that R.sup.1 is different from iodine, when R.sup.2 is hydroxy or benzoyloxy, R.sup.3 is hydrogen, R.sup.4 is unsubstituted phenyl, R.sup.5 is hydrogen, m stands for zero, X is O, and Y is a direct bond,and tautomers thereof, which possess antiviral activity and can therefore be used in the form of medicaments for the control and prevention of viral infections are described. The compounds of formula I can be prepared according to known methods.

    Pyrazolo [1,2-a][1,2]-diazepines useful as antihypertensives
    5.
    发明授权
    Pyrazolo [1,2-a][1,2]-diazepines useful as antihypertensives 失效
    吡唑并[1,2-a] [1,2] - 二氮杂作为抗高血压药物

    公开(公告)号：US4658024A

    公开(公告)日：1987-04-14

    申请号：US697559

    申请日：1985-02-01

    申请人： Michael R. Attwood ,  Cedric H. Hassall ,  Robert W. Lambert ,  Geoffrey Lawton ,  Sally Redshaw

    发明人： Michael R. Attwood ,  Cedric H. Hassall ,  Robert W. Lambert ,  Geoffrey Lawton ,  Sally Redshaw

    IPC分类号： C07D209/48 ,  C07D231/04 ,  C07D237/04 ,  C07D403/06 ,  C07D487/04 ,  C07F9/38 ,  C07F9/40 ,  C07F9/6509 ,  C07F9/6561 ,  C07K5/078 ,  C07D403/04 ,  A61K31/33 ,  C07D401/04

    CPC分类号： C07D209/48 ,  C07D231/04 ,  C07D237/04 ,  C07D403/06 ,  C07D487/04 ,  C07F9/3886 ,  C07F9/409 ,  C07F9/650947 ,  C07F9/6561 ,  C07K5/06139

    摘要： Novel compounds of the formula ##STR1## wherein B represents a methylene, ethylene or vinylene group, R.sup.1 represents a hydrogen atom or an alkyl, aralkyl, amino-alkyl, mono-alkylamino-alkyl, dialkylamino-alkyl, acylamino-alkyl, phthalimido-alkyl, alkoxycarbonylamino-alkyl, aryloxycarbonylamino-alkyl, aralkoxycarbonylamino-alkyl, alkylaminocarbonylamino-alkyl, arylaminocarbonylamino-alkyl, aralkylaminocarbonylamino-alkyl, alkylsulphonylamino-alkyl or arylsulphonylamino-alkyl group, R.sup.2 represents a carboxyl, alkoxycarbonyl or aralkoxycarbonyl group or a group of the formula ##STR2## R.sup.3 represents a carboxyl, alkoxycarbonyl or aralkoxycarbonyl group, R.sup.4 and R.sup.5 each represent a hydrogen atom or R.sup.4 and R.sup.5 together represent an oxo group, R.sup.6 and R.sup.7 each represent a hydrogen atom or an alkyl or aralkyl group or R.sup.6 and R.sup.7 together with the nitrogen atom to which they are attached represent a 5-membered or 6-membered heteromonocyclic ring which may contain a further nitrogen atom or an oxygen or sulphur atom, and n stands for zero, 1 or 2, and pharmaceutically acceptable salts thereof have antihypertensive activity and can be used as medicaments in the form of pharmaceutical preparations.

    摘要翻译： 新颖的式Ⅰ化合物，其中B代表亚甲基，亚乙基或亚乙烯基，R 1表示氢原子或烷基，芳烷基，氨基 - 烷基，单烷基氨基 - 烷基，二烷基氨基 - 烷基，酰氨基 - 烷基，邻苯二甲酰亚氨基 烷基，烷氧基羰基氨基 - 烷基，烷基氨基羰基氨基 - 烷基，芳基氨基羰基氨基 - 烷基，芳烷基氨基羰基氨基 - 烷基，烷基磺酰基氨基 - 烷基或芳基磺酰基氨基 - 烷基， 式中，R 3表示羧基，烷氧基羰基或芳烷氧基羰基，R 4和R 5各自表示氢原子或R 4，R 5一起表示氧代基，R 6和R 7各自表示氢原子或烷基或芳烷基，或者R 6和R 7 与它们所连接的氮原子一起表示可以含有另外的氮原子或氧的5元或6元杂单环，或 硫原子，n表示0,1或2，其药学上可接受的盐具有抗高血压活性，可用作药物制剂形式的药物。

    Acyl derivatives
    6.
    发明授权
    Acyl derivatives 失效
    酰基衍生物

    公开(公告)号：US4250085A

    公开(公告)日：1981-02-10

    申请号：US971156

    申请日：1978-12-20

    申请人： Frank R. Atherton ,  Michael J. Hall ,  Cedric H. Hassall ,  Robert W. Lambert ,  Peter S. Ringrose

    发明人： Frank R. Atherton ,  Michael J. Hall ,  Cedric H. Hassall ,  Robert W. Lambert ,  Peter S. Ringrose

    IPC分类号： C07K5/04 ,  A61K38/00 ,  A61P31/04 ,  C07F9/38 ,  C07K1/113 ,  C07K5/06 ,  C07K5/08 ,  C07C103/52 ,  A61K37/00 ,  C07G7/00

    CPC分类号： C07K5/0827 ,  C07F9/3808 ,  C07K5/06191 ,  A61K38/00 ,  Y02P20/55 ,  Y10S930/27

    摘要： Peptide derivatives provided by the present invention are compounds of the general formula ##STR1## wherein R.sup.1 represents a hydrogen atom or the methyl or hydroxymethyl group or a mono-, di- or trihalomethyl mgroup; R.sup.2 represents the characterizing group of an .alpha.-amino acid of the type normally found in proteins or a lower alkyl or hydroxy- (lower alkyl) group other than the characterising group of an .alpha.-amino acid of the type normally found in proteins; R.sup.3 represents a lower alkyl, lower cycloalkyl, lower alkenyl, aryl or aryl-(lower alkyl) group; R.sup.4 represents a hydrogen atom or a lower alkyl group; n stands for 1,2 or 3; the configuration at the carbon atom designated as (a) is (R) when R.sup.1 represents other than a hydrogen atom and the configuration at the carbon atom designated as (b) is (L) when R.sup.2 represents other than a hydrogen atom, and pharmaceutically acceptable salts thereof.The compounds exhibit activity as antibacterial agents against a range of gram-positive and gram-negative bacteria. Also disclosed are intermediates and a process for the production of the end product.

    摘要翻译： 本发明提供的肽衍生物是通式为“IMAGE”的化合物，其中R 1表示氢原子或甲基或羟甲基或单，二或三卤甲基基团; R2代表通常存在于蛋白质中的α-氨基酸的表征基团或除通常在蛋白质中发现的α-氨基酸的特征基团以外的低级烷基或羟基 - （低级烷基）基团; R3表示低级烷基，低级环烷基，低级烯基，芳基或芳基 - （低级烷基）基团; R4代表氢原子或低级烷基; n代表1,2或3; 当R 1表示除氢原子之外时，指定为（a）的碳原子上的构型为（R），当R 2表示氢原子以外，以（b）表示的碳原子上的构型为（L） 其可接受的盐。 该化合物表现出针对一系列革兰氏阳性和革兰氏阴性细菌的抗菌剂的活性。 还公开了中间体和用于生产最终产品的方法。

    Pyrimidine derivatives
    8.
    发明授权
    Pyrimidine derivatives 失效
    嘧啶衍生物

    公开(公告)号：US4882316A

    公开(公告)日：1989-11-21

    申请号：US79741

    申请日：1987-07-30

    申请人： Robert W. Lambert ,  Joseph A. Martin ,  Gareth J. Thomas

    发明人： Robert W. Lambert ,  Joseph A. Martin ,  Gareth J. Thomas

    IPC分类号： C07D405/06 ,  A61K31/505 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7064 ,  A61K31/7068 ,  A61K31/7072 ,  A61P31/12 ,  C07D405/04 ,  C07H19/06 ,  C12N9/99

    CPC分类号： C07H19/06

    摘要： Compounds of the formula ##STR1## wherein R.sup.1 is halogen, C.sub.1-4 -alkyl or halo-(C.sub.1-4 - alkyl), R.sup.2 is hydrogen, hydroxy or acyloxy, R.sup.3 and R.sup.4 each are hydrogen or C.sub.1-4 -alkyl, R.sup.5 is aryl or aryloxy, X is O or NH and Y is --CO--CH.sub.2 --, --CH(OH)--CH.sub.2 --, --CH.sub.2 --CH.sub.2 --, --S--, --SO-- or --SO.sub.2 --,and tautomers thereof are described. Compounds of formula I and their tautomers possess antiviral activity and can be used in the form of medicaments for the control and prevention of viral infections.

    摘要翻译： 其中R 1是卤素，C 1-4 - 烷基或卤代（C 1-4 - 烷基），R 2是氢，羟基或酰氧基，R 3和R 4各自是氢或C 1-4 - 烷基， R5是芳基或芳氧基，X是O或NH，Y是-CO-CH2-，-CH（OH）-CH2-，-CH2-CH2-，-S-，-SO-或-SO2-，及其互变异构体 被描述。 式I化合物及其互变异构体具有抗病毒活性，可用于控制和预防病毒感染的药物形式。

    Pyridazo[1,2-a][1,2]diazepines
    9.
    发明授权
    Pyridazo[1,2-a][1,2]diazepines 失效
    哒唑[1,2-a] [1,2]二氮杂

    公开(公告)号：US4512924A

    公开(公告)日：1985-04-23

    申请号：US493876

    申请日：1983-05-12

    申请人： Michael R. Attwood ,  Cedric H. Hassall ,  Robert W. Lambert ,  Geoffrey Lawton ,  Sally Redshaw

    发明人： Michael R. Attwood ,  Cedric H. Hassall ,  Robert W. Lambert ,  Geoffrey Lawton ,  Sally Redshaw

    IPC分类号： C07D209/48 ,  C07D231/04 ,  C07D237/04 ,  C07D403/06 ,  C07D487/04 ,  C07F9/38 ,  C07F9/40 ,  C07F9/6509 ,  C07F9/6561 ,  C07K5/078

    CPC分类号： C07D209/48 ,  C07D231/04 ,  C07D237/04 ,  C07D403/06 ,  C07D487/04 ,  C07F9/3886 ,  C07F9/409 ,  C07F9/650947 ,  C07F9/6561 ,  C07K5/06139

    摘要： Novel compounds of the formula ##STR1## wherein B represents a methylene, ethylene or vinylene group, R.sup.1 represents a hydrogen atom or an alkyl, aralkyl, amino-alkyl, mono-alkylamino-alkyl, dialkylaminoalkyl, acylamino-alkyl, phthalimido-alkyl, alkoxycarbonylamino-alkyl, aryloxycarbonylamino-alkyl, aralkoxycarbonylamino-alkyl, alkylaminocarbonylamino-alkyl, arylaminocarbonylamino-alkyl, aralkylaminocarbonylamino-alkyl, alkylsulphonylamino-alkyl or arylsulphonylamino-alkyl group, R.sup.2 represents a carboxyl, alkoxycarbonyl or aralkoxycarbonyl group or a group of the formula ##STR2## R.sup.3 represents a carboxyl, alkoxycarbonyl or aralkoxycarbonyl group, R.sup.4 and R.sup.5 each represent a hydrogen atom or R.sup.4 and R.sup.5 together represent an oxo group, R.sup.6 and R.sup.7 each represent a hydrogen atom or an alkyl or aralkyl group or R.sup.6 and R.sup.7 together with the nitrogen atom to which they are attached represent a 5-membered or 6-membered heteromonocyclic ring which may contain a further nitrogen atom or an oxygen or sulphur atom, and n stands for zero, 1 or 2,and pharmaceutically acceptable salts thereof have antihypertensive activity and can be used as medicaments in the form of pharmaceutical preparations.

    摘要翻译： 新颖的式Ⅰ化合物，其中B代表亚甲基，亚乙基或亚乙烯基，R1代表氢原子或烷基，芳烷基，氨基 - 烷基，单烷基氨基 - 烷基，二烷基氨基烷基，酰氨基 - 烷基，邻苯二甲酰亚氨基 - 烷基 烷氧基羰基氨基 - 烷基，芳氧基羰基氨基 - 烷基，烷基氨基羰基氨基 - 烷基，芳基氨基羰基氨基 - 烷基，芳烷基氨基羰基氨基 - 烷基，烷基磺酰基氨基 - 烷基或芳基磺酰基氨基 - 烷基，R2表示羧基， 图示> R3表示羧基，烷氧基羰基或芳烷氧基羰基，R4和R5各自表示氢原子或R4和R5一起表示氧代基，R6和R7各自表示氢原子或烷基或芳烷基或R6和R7连同 它们所连接的氮原子表示可以含有另外的氮原子或氧的5元或6元杂环， 硫原子，n表示0,1或2，其药学上可接受的盐具有抗高血压活性，可用作药物制剂形式的药物。